立体选择性合成（S，S）－2－羟基－3－氨基－4－苯基丁酸  

On diastereoselective synthesis of drugs:proparation of (s,s)-2-hydroxyl-3-amino-4-phenyl bytyric acid

作　　者：肖敏[1] 吴筱屏[1] 梁本熹[1] 长谷川Y 松本S 村松Y 李志良[1] 

机构地区：[1]湖南大学化学化工系,东京药物所开发部,日本国立技科大学工学院,早稻田大学理学院

出　　处：《化学试剂》1996年第6期324-326,336,共4页Chemical Reagents

基　　金：国家自然科学基金

摘　　要：研究了药物及其中间体的立体选择性合成。报道了一种抗艾滋病候选药中间体（Ｓ，Ｓ）－２－羟基－３－氨基－４－笨基丁酸的立体选择性合成方法，显著地提高了Ｓ－型产物的收率。Systematic investigation was made on diastereoselective organic synthesis of drugs. In this paper, (S,S)-2-hydroxyl-3-amino-4-pheny butyric acid (HAPBA) as a core pharmacophore unit of anti-AIDS HIVprotease, called allophenylnorstatine (APN), was synthesized diastereoselectively by modifying the originalsynthetic pathway to a novel route based on the Grams asymmetric induction. The ratio of the desired (S,S )-product to the undesired (R,S )-product was raisedfrom 43% to 68%,with e. e% = 35 %,in this proposedorganic synthesis procedure.

关 键 词：药物立体选择性 羟基氨基酸 抗艾滋病药 

分 类 号：TQ463.25[化学工程—制药化工]